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Related Concept Videos

Routes of Drug Administration: Enteral01:18

Routes of Drug Administration: Enteral

Medications can be administered through the enteral route using liquids, capsules, or tablets.
Enteral administration involves drug administration via the mouth in two ways: orally or sublingually.
Unlike sublingually drugs, drugs that are taken orally pass through the gastrointestinal (GI) tract and get metabolized by the liver. Once metabolized, the drug is absorbed into the systemic circulation, reaching different body parts via the bloodstream. However, while passing through the stomach,...
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Drug Absorption: Factors Affecting GI Absorption

The process of oral drug absorption can be influenced by several factors. Weakly acidic drugs tend to be absorbed more readily from the stomach due to their nonionized state. However, absorption may be less efficient in the upper intestine, where drugs are often ionized. Interestingly, despite the stomach's apparent advantage for drug absorption, its mucous layer can hinder diffusion. Its surface area is also smaller than the intestine's, which can further slow down the absorption rate.
In...
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Drugs for Treatment of Constipation-Predominant IBS

Pharmacological therapies for IBS-C are designed to alleviate abdominal discomfort and enhance bowel function. In patients with IBS-C, fiber supplements may help soften stools and decrease straining, but may also lead to increased gas production and bloating. Osmotic laxatives like milk of magnesia are frequently used to soften stools and increase stool frequency in IBS-C patients. In addition, two drugs approved for use in severe IBS-C adult cases are linaclotide (Linzess) and lubiprostone...
Drug Absorption: Overview01:17

Drug Absorption: Overview

The process of drug absorption signifies the transition of a drug from its site of administration into the plasma. This process is influenced by various factors, including the route of administration, the anatomy of the absorption site, the mechanism of absorption, gut motility, and the drug's physicochemical properties.
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Drug Delivery: Enteral Route01:18

Drug Delivery: Enteral Route

The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
Drugs in...
Non-Oral Extravascular Drug Absorption Routes01:15

Non-Oral Extravascular Drug Absorption Routes

Non-oral extravascular routes, which encompass sublingual, buccal, topical, intramuscular, and inhalation methods, primarily utilize passive diffusion to transport drugs into the systemic circulation. The absorption rates and effectiveness of these routes depend on the drug's physicochemical properties, as well as the patient's anatomical and pathophysiological state.
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more effectively...

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Slow-release Drug Delivery through Elvax 40W to the Rat Retina: Implications for the Treatment of Chronic Conditions
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Rectal absorption of lamotrigine compressed tablets.

A K Birnbaum1, R L Kriel, R T Burkhardt

  • 1Experimental and Clinical Pharmacology and Medicinal Chemistry, Epilepsy Research and Education Program, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota 55455, USA. birnb002@tc.umn.edu

Epilepsia
|July 18, 2000
PubMed
Summary

Rectal administration of lamotrigine (LTG) compressed tablets is possible, but absorption is less extensive and slower compared to oral dosing. This study evaluated the pharmacokinetics of rectal versus oral LTG in healthy volunteers.

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Area of Science:

  • Pharmacology
  • Clinical Pharmacy
  • Drug Delivery Systems

Background:

  • Oral drug administration can be interrupted, posing challenges for antiepileptic drugs lacking parenteral formulations.
  • Rectal administration offers a viable alternative when oral intake is not feasible, provided the drug is absorbed rectally.
  • Lamotrigine (LTG) is an antiepileptic drug where rectal administration could be clinically important.

Purpose of the Study:

  • To compare the single-dose pharmacokinetics of lamotrigine (LTG) compressed tablets following rectal versus oral administration.
  • To assess the bioavailability of rectally administered LTG in healthy volunteers.
  • To determine the rate and extent of LTG absorption via the rectal route.

Main Methods:

  • A single-dose, two-period crossover study involving 12 healthy volunteers.
  • Administration of a 100 mg LTG compressed tablet orally and rectally (crushed and suspended in 10 mL water) after a 2-week washout period.
  • Collection of plasma samples for 120 hours post-dose and analysis of LTG concentrations using a developed HPLC method.

Main Results:

  • LTG plasma concentrations were significantly lower after rectal administration compared to oral administration.
  • The average area under the curve (AUC) for rectal LTG was 28.90 ± 9.5 μg/mL/hr, versus 51.71 ± 19.2 μg/mL/hr for oral LTG.
  • The average maximum LTG concentration (Cmax) was 0.53 ± 0.14 μg/mL rectally and 1.45 ± 0.35 μg/mL orally, with a relative bioavailability of 0.63 ± 0.33 for the rectal route.

Conclusions:

  • Lamotrigine suspension prepared from compressed tablets is absorbed rectally.
  • Rectal absorption of LTG is less extensive and slower than oral absorption.
  • No drug-related rashes or serious adverse events were reported during the study.